hnRNPK-IN-1 是一种异质核糖核蛋白 K (hnRNPK) 结合配体，用 SPR 和 MST 测量的Kd值分别为 4.6 μM 和 2.6 μM。hnRNPK-IN-1 通过破坏 hnRNPK 和 c-myc 启动子的结合来抑制 c-myc 转录。hnRNPK-IN-1诱导 Hela 细胞凋亡 (apoptosis)，并具有很强的抗肿瘤活性。
| 生物活性 | hnRNPK-IN-1 is aheterogeneous nuclear ribonucleoprotein K (hnRNPK)binding ligand withKdvalues of 4.6 μM and 2.6 μM measured with SPR and MST, respectively. hnRNPK-IN-1 inhibitsc-myctranscription by disrupting the binding of hnRNPK andc-mycpromoter. hnRNPK-IN-1 induces Hela cellsapoptosisand has strongly anti-tumor activities[1]. |
| IC50& Target | Kd: 4.6 μM (hnRNPK; SPR assay) and 2.6 μM (hnRNPK; MST assay)[1] |
体外研究
(In Vitro) | hnRNPK-IN-1 (Compound 25; 1.25-5 μM; 24 hours) treatment induces Hela cells apoptosis could be due to its repression of cmyc transcription[1].
hnRNPK-IN-1 (1.25-5 μM; 48 hours) treatment down-regulates c-myc gene transcription and expression in Hela cells in a dose-dependent manner[1].
hnRNPK-IN-1 shows a selective anti-proliferative effect on human cancer cell lines (Siha, A549, Hela, U2OS, A375, HuH7 and HEK293 cells) with IC50 values ranged from 1.36 to 3.59 μM[1].
hnRNPK-IN-1 could selectively bind to hnRNP K without significant interaction with c-myc promoter DNA. The binding of hnRNPK-IN-1 to hnRNP K could disrupt the interaction between hnRNP K and c-myc promoter DNA in vitro and in cells[1].
Apoptosis Analysis[1] | Cell Line: | Hela cells | | Concentration: | 1.25 μM, 2.5 μM, 5 μM | | Incubation Time: | 24 hours | | Result: | Induced Hela cells apoptosis and apoptosis-related protein expressions. |
RT-PCR[1] | Cell Line: | Hela cells | | Concentration: | 1.25 μM, 2.5 μM, 5 μM | | Incubation Time: | 48 hours | | Result: | Caused a reduction of c-myc mRNA in a dose-dependent manner in Hela cells. |
Western Blot Analysis[1] | Cell Line: | Hela cells | | Concentration: | 1.25 μM, 2.5 μM, 5 μM | | Incubation Time: | 48 hours | | Result: | The expression levels of c-MYC also decreased in a dose-dependent manner. |
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体内研究
(In Vivo) | hnRNPK-IN-1 (Compound 25; 6.7-20 mg/kg; i.p.; once a day; for three weeks) exhibits good tumor growth inhibition in a Hela xenograft tumor model[1].
| Animal Model: | BALB/c female nude mice (five weeks old) bearing Hela cells[1] | | Dosage: | 6.7 mg/kg, 20 mg/kg | | Administration: | Intraperitoneal injection; once a day; for three weeks | | Result: | Inhibited tumor growth in a Hela cervical xenograft. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | 4°C | 2 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: DMSO : 5 mg/mL(11.92 mM;ultrasonic and warming and heat to 80℃) 配制储备液 | 1 mM | 2.3842 mL | 11.9209 mL | 23.8419 mL | | 5 mM | 0.4768 mL | 2.3842 mL | 4.7684 mL | | 10 mM | 0.2384 mL | 1.1921 mL | 2.3842 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 |
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